A safe, reliable and scalable process for the preparation of N-Boc-2-tert-butyldimethylsiloxy- pyrrole (TBSOP) is described. In a three-step, one-pot sequence (±)-4-amino-3- hydroxybutyric acid was converted to N-Boc-4-hydroxy-2-pyrrolidinone. This stable crystalline product was isolated by filtration directly from the reaction mixture. Dehydration followed by enolization and silylation produced the target compound without the need for ...
